The present invention is directed toward pyrazolopyrimidine (Formula 1) and pyrimidinyl (Formula 2) bisphosphonic esters, acids, and their pharmaceutically acceptable salts which are useful as anti-inflammatories and anti-arthritic agents.
The present compounds, unlike other anti-inflammatory agents, are not prostaglandin synthetase inhibitors. Typically, prostaglandin synthetase activity is inhibited by nonsteroidal anti-inflammatory agents and many of their actions, including side effects, have been attributed to this inhibition of prostaglandin synthesis. The subject compounds still possess anti-inflammatory response without suppressing the production of prostaglandin. This can be an advantage because it is known that at high concentrations prostaglandins are considered anti-inflammatory. The subject compounds are also useful for treating arthritis and its related symptoms such as inflammation and prevention of excessive bone regrowth and remodeling.